Patent SG-11201407999T-A (SG)
Title: ICMT Inhibitors
Inventor: RAMANUJULU PONDY MURUGAPPAN
IPC: C07D401/10
Filed: 2013-05-30
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 5 December 2013 (05.12.2013) WIPOIPCT (10) International Publication Number WO 2013/180656 A1 (51) International Patent Classification: C07D 209/14 (2006.01) C07D 471/04 (2006.01) C07D 401/10 (2006.01) C07D 403/10 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/SG2013/000219 30 May 2013 (30.05.2013) English English (30) Priority Data: 201204064-8 1 June 2012 (01.06.2012) SG (71) Applicant: NATIONAL UNIVERSITY OF SINGA­ PORE [SG/SG]; 21 Lower Kent Ridge Road, Singapore 119077 (SG). (72) Inventors: RAMANUJULU, Pondy Murugappan; De­ partment of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543 (SG). YANG, Tianming; Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543 (SG). CASEY, Mei-Wang; Duke NUS Graduate Medical School, 8,College Road, Singapore 169857 (SG). CASEY, Patrick J; Duke NUS Graduate Medical School, 8,College Road, Singapore 169857 (SG). GO, Mei Lin; Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543 (SG). (74) Agent: SPRUSON & FERGUSON (ASIA) PTE LTD; P.O. Box 1531, Robinson Road Post Office, Singapore 903031 (SG). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 21(3)) V© ^© o 00 i-H en i-H o CJ (54) Title: ICMT Inhibitors (57) Abstract: The invention provides a 1,3,5-substituted indole wherein the substituent position at 1 is a C6 to C12 alkyl group; the substituent at position 3 is CH NR'R 2 2 wherein R is H 1 or CI to C3 alkyl, R 1 being optionally substituted with -OH, -SH, -NH 2 or NHalkyl, wherein alkyl is a CI to C4 alkyl group, and R 2 is CI to C3 alkyl or (CH)„ 2 bonded to position 2 of the indole, wherein n is 1, 2 or 3; and the substituent at position 5 is either an optionally substituted nitrogen containing heteroaromatic ring or an aminosulf- onylphenyl group or an alkylsulfonylphenyl group.